RI-2
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 44.17 μM
同源重组(HR)是细胞中的重要过程,提供了阻断DNA复制的DNA双链断裂和病变的修复.RAD51是一种进化上保守的蛋白,是HR的中心.在癌细胞中,RAD51蛋白的过表达十分常见,是肿瘤治疗的潜在靶标.RI-2是优化的可逆RAD51抑制剂.
体外实验:尽管与RI-1相比,RI-2的活性相对降低,但在基于细胞的MMC实验中,RI-2保留了对敏感细胞足够的活性.RI-2孵育24小时后,对谷胱甘肽没有反应性.洗脱之前使用RI-2处理RAD51蛋白,产生不可测量的DNA结合活性丧失,尽管RI-2是已知的可以抑制RAD51活性的物质,IC50为44.17 μM.这表明,RI-2对RAD51的抑制是完全可逆的[1].
在体实验:RI-1是RI-2的类似物,易化了已知晶体结构的RAD51结合口袋的映射,RI-1的这种反应可能会限制其在临床前动物模型中的应用.在含硫醇的溶液中的反应表明,RI-1半衰期相对较短[1].
临床试验:到目前为止,RI-2还处于临床前开发阶段.
参考文献:
[1] Budke B, Kalin JH, Pawlowski M, Zelivianskaia AS, Wu M, Kozikowski AP, Connell PP. An optimized RAD51 inhibitor that disrupts homologous recombination without requiring Michael acceptor reactivity. J Med Chem. 2013 Jan 10;56(1):254-63.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 433.28 |
Cas No. | 1417162-36-7 |
Formula | C21H18Cl2N2O4 |
Solubility | ≥21.65 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
Chemical Name | 1-(3,4-dichlorophenyl)-3-(4-methoxyphenyl)-4-morpholino-1H-pyrrole-2,5-dione |
SDF | Download SDF |
Canonical SMILES | COC1=CC=C(C(C(N2C3=CC(Cl)=C(Cl)C=C3)=O)=C(N4CCOCC4)C2=O)C=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |